Tchem HIF1A Hypoxia-inducible factor 1-alpha

Protein Summary

Description

Functions as a master transcriptional regulator of the adaptive response to hypoxia. Under hypoxic conditions, activates the transcription of over 40 genes, including erythropoietin, glucose transporters, glycolytic enzymes, vascular endothelial growth factor, HILPDA, and other genes whose protein products increase oxygen delivery or facilitate metabolic adaptation to hypoxia. Plays an essential role in embryonic vascularization, tumor angiogenesis and pathophysiology of ischemic disease. Heterodimerizes with ARNT; heterodimer binds to core DNA sequence 5'-TACGTG-3' within the hypoxia response element (HRE) of target gene promoters (By similarity). Activation requires recruitment of transcriptional coactivators such as CREBBP and EP300. Activity is enhanced by interaction with both, NCOA1 or NCOA2. Interaction with redox regulatory protein APEX seems to activate CTAD and potentiates activation by NCOA1 and CREBBP. Involved in the axonal distribution and transport of mitochondria in neurons during hypoxia. This gene encodes the alpha subunit of transcription factor hypoxia-inducible factor-1 (HIF-1), which is a heterodimer composed of an alpha and a beta subunit. HIF-1 functions as a master regulator of cellular and systemic homeostatic response to hypoxia by activating transcription of many genes, including those involved in energy metabolism, angiogenesis, apoptosis, and other genes whose protein products increase oxygen delivery or facilitate metabolic adaptation to hypoxia. HIF-1 thus plays an essential role in embryonic vascularization, tumor angiogenesis and pathophysiology of ischemic disease. Alternatively spliced transcript variants encoding different isoforms have been identified for this gene. [provided by RefSeq, Jul 2011]

Uniprot Accession IDs

• Q16665
• C0LZJ3
• Q53XP6
• Q96PT9
• Q9UPB1
• HIF-1-alpha

Gene Name

• HIF1A

Ensembl ID

• ENST00000323441
• ENSP00000323326
• ENSG00000100644
• ENST00000337138
• ENSP00000338018
• ENST00000539097
• ENSP00000437955

Symbol

• BHLHE78
• MOP1
• PASD8
• HIF1
• MOP1
• PASD8
• HIF-1A
• bHLHe78
• HIF-1alpha
• HIF1-ALPHA
• HIF-1-alpha

Knowledge Table

Most Knowledge About	Knowledge Value (0 to 1 scale)
biological process	1
chemical	1
hub protein	1
disease perturbation	0.97
molecular function	0.97

Protein Classes

PANTHER Classes

Protein / Transcription Factor / Basic Helix-loop-helix Transcription Factor / Hypoxia-inducible Factor 1-alpha

Protein / Nucleic Acid Binding / Hypoxia-inducible Factor 1-alpha

DTO Classes

Protein / Transcription Factor / Basic Helix-loop-helix Transcription Factor / Hypoxia-inducible Factor 1-alpha

IDG Development Level Summary

Tdark

These are targets about which virtually nothing is known. They do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 12164.25   (req: < 5)

Gene RIFs: 3439   (req: <= 3)

Antibodies: 2061   (req: <= 50)

Tbio

These targets do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 12164.25   (req: >= 5)

Gene RIFs: 3439   (req: > 3)

Antibodies: 2061   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 97

Tchem

Target has at least one ChEMBL compound with an activity cutoff of < 30 nM - AND - satisfies the preceding conditions

Active Ligands: 90

Tclin

Target has at least one approved drug - AND - satisfies the preceding conditions

Active Drugs: 2